منابع مشابه
A Novel G q / 11 - selective Inhibitor *
YM-254890, which was isolated from the culture broth of Chromobacterium sp., inhibits ADP-induced platelet aggregation and has antithrombotic and thrombolytic effects. YM-254890 blocks G q/11-coupled ADP receptor P2Y1-mediated Ca mobilization. Here we report that YM-254890 is a selective G q/11 inhibitor. YM-254890 blocked Ca mobilization mediated by several G q/11coupled receptors but not by G...
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Signal Transduction Team, Section of Cell and Molecular Biology, The Institute of Cancer Research, 237 Fulham Road, London, SW3 6JB, UK. Gene and Oncogene Targeting Team, Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey, SM2 5NG, UK. Molecular Pathology Team, The Breakthrough Breast Cancer Research Centre, The Institute of Can...
متن کاملA novel, selective, and efficacious nanomolar pyridopyrazinone inhibitor of V600EBRAF.
Oncogenic BRAF is a critical driver of proliferation and survival and is thus a validated therapeutic target in cancer. We have developed a potent inhibitor, termed 1t (CCT239065), of the mutant protein kinase, (V600E)BRAF. 1t inhibits signaling downstream of (V600E)BRAF in cancer cells, blocking DNA synthesis, and inhibiting proliferation. Importantly, we show that 1t is considerably more sele...
متن کاملNovel Binding Mode of a Potent and Selective Tankyrase Inhibitor
Tankyrases (TNKS1 and TNKS2) are key regulators of cellular processes such as telomere pathway and Wnt signaling. IWRs (inhibitors of Wnt response) have recently been identified as potent and selective inhibitors of tankyrases. However, it is not clear how these IWRs interact with tankyrases. Here we report the crystal structure of the catalytic domain of human TNKS1 in complex with IWR2, which...
متن کاملKDM4B as a Target for Prostate Cancer: Structural Analysis and Selective Inhibition by a Novel Inhibitor
The KDM4/JMJD2 Jumonji C-containing histone lysine demethylases (KDM4A-KDM4D), which selectively remove the methyl group(s) from tri/dimethylated lysine 9/36 of H3, modulate transcriptional activation and genome stability. The overexpression of KDM4A/KDM4B in prostate cancer and their association with androgen receptor suggest that KDM4A/KDM4B are potential progression factors for prostate canc...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 2004
ISSN: 0021-9258
DOI: 10.1074/jbc.m408846200